Reaction Details |
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Target | Potassium voltage-gated channel subfamily H member 2 |
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Ligand | BDBM50603097 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2243007 (CHEMBL5157217) |
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IC50 | <50119±n/a nM |
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Citation | Humphreys, PG; Atkinson, SJ; Bamborough, P; Bit, RA; Chung, CW; Craggs, PD; Cutler, L; Davis, R; Ferrie, A; Gong, G; Gordon, LJ; Gray, M; Harrison, LA; Hayhow, TG; Haynes, A; Henley, N; Hirst, DJ; Holyer, ID; Lindon, MJ; Lovatt, C; Lugo, D; McCleary, S; Molnar, J; Osmani, Q; Patten, C; Preston, A; Rioja, I; Seal, JT; Smithers, N; Sun, F; Tang, D; Taylor, S; Theodoulou, NH; Thomas, C; Watson, RJ; Wellaway, CR; Zhu, L; Tomkinson, NCO; Prinjha, RK Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate. J Med Chem65:2262-2287 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Potassium voltage-gated channel subfamily H member 2 |
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Name: | Potassium voltage-gated channel subfamily H member 2 |
Synonyms: | 1,3-beta-glucan synthase component GLS2 | Cytochrome P450 3A4 | ERG | ERG1 | Eag-related protein 1 | Ether a-go-go related gene potassium channel (hERG) | Ether-a-go-go-related gene (HERG) | Ether-a-go-go-related gene potassium channel (hERG) | Ether-a-go-go-related gene potassium channel 1 | Ether-a-go-go-related gene potassium channel 1 (HERG) | Ether-a-go-go-related gene potassium channel 1 (hERG1) | Ether-a-go-go-related protein (hERG) | Ether-a-go-go-related protein 1 | Ether-a-go-go-related protein 1 (HERG) | H-ERG | HERG | KCNH2 | KCNH2_HUMAN | Potassium voltage-gated channel subfamily H member 2 (hERG) | Transcriptional regulator ERG | Voltage-gated potassium channel subunit Kv11.1 | eag homolog | hERG Potassium Channel 1 | putative potassium channel subunit |
Type: | Multi-pass membrane protein |
Mol. Mass.: | 126672.65 |
Organism: | Homo sapiens (Human) |
Description: | Q12809 |
Residue: | 1159 |
Sequence: | MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
QLGALTSQPLHRHGSDPGS
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BDBM50603097 |
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n/a |
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Name | BDBM50603097 |
Synonyms: | CHEMBL5195288 |
Type | Small organic molecule |
Emp. Form. | C17H18ClN5O2 |
Mol. Mass. | 359.81 |
SMILES | C[C@H]1C[C@@H](Nc2ncc(Cl)cn2)c2cc(ccc2N1C(C)=O)C(N)=O |r| |
Structure |
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